| 摘要 |
<p>PURPOSE: To obtain the new compound having a strong cathepsin L-inhibiting action and a bone absorption-inhibiting action and useful as a thiolprotease- inhibiting agent and a agent for preventing and treating bone diseases such as osteoporosis. CONSTITUTION: This compound is expressed by formula I [R1 is carboxyl; X is divalent hydrocarbon residue; R2 is H, hydrocarbon residue; R3 is alkyl substituted with a group formed through an O or S(O)n (n is 0-2), but when the group of formula: -NH-X-CO- is a leucine residue, R3 is not 3-or 4-hydroxy-3- methylbuty]l, e.g. N-[N-[(2S,3S)-3-trans-ethoxycarbonyloxirane-2-carbonyl]-L- phenylalanyl]-1-amino-3-methoxypropane. The compound is obtained by reacting a compound (salt) of formula II with a compound (salt) of formula III by an usual peptide synthetic method such as a liquid phase synthetic method, a solid phase synthetic method, etc., and further, if necessary, subjecting the reaction product to a protecting group-removing reaction.</p> |
